Prolonged Release of Anti-Retroviral Efavirenz From System Using ZIF-8 as Carrier

Abstract

Background: Acquired Immunodeficiency Syndrome (AIDS) is a major public health problem in the world. One of the highly effective drugs in anti-HIV therapy is efavirenz (EFZ), which is classified as Class II according to the Classification System of Biopharmaceuticals, presenting low solubility and high permeability, this being an obstacle related to the drug.

Objective: This study aimed to obtain an innovative system based on EFZ and the Zeolitic Imidazolate Framework (ZIF-8) to use in the development of prolonged-release pharmaceutical forms that can circumvent this problem.

Methods: The EFZ: ZIF-8 system was obtained by a selected ex-situ method due to its higher incorporation efficiency. Different characterization techniques corroborated the obtainment of the system, and drug release was analyzed by dissolution testing under sink conditions, the profiles being adjusted to some kinetic models.

Results: At pH 1.2, the structure of ZIF-8 breaks down rapidly, releasing a large amount of drug within either 3h or short time. In the pH 4.5 and 6.8 medium, the EFZ release from the EFZ: ZIF-8 system obtained in ethanol was prolonged, releasing 95% of the drug in 24h at pH 4.5 and 75% medium at pH 6.8.

Conclusion: It is evident that a promising pH-sensitive system was obtained using ZIF-8 as a novel carrier of EFZ intended for the alternative treatment of AIDS.

Keywords: AIDS; HIV; anti-HIV agents; dissolution; drug release; metal-organic frameworks.